Abstract
The effective identification, selection, and implementation of small molecules for the interrogation of biological systems require an intricate understanding of the chemical principles underlying their cellular activities. While much has been published regarding the use of screening techniques in forward chemical genetics platforms and on small-molecule target identification, less emphasis has been placed on detailed strategies for evaluating, selecting, and optimizing screening hits. This chapter provides practical tools for identifying and developing promising screening hit compounds into effective tools for biological discovery.
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